Mechanisms of action of naturally occurring irreversible enzyme inhibitors

Silicon in synthesis: stabase adducts - a new primary amine protecting group: alkylation of ethyl glycinate

The Clarke-Carbon clone bank of hybrid plasmid Escherichia coli DNA has been screened for plasmids able to complement an E. coli strain deficient for the production of beta-cystathionase. Clone 4-14 had the ability to complement a deletion mutation at this locus and expressed higher levels of beta-cystathionase than the wild-type strain. The transfer of the plasmid carried by this clone to a strain that constitutively expresses all the enzymes of the methionine biosynthetic pathway results in 100-fold overproduction of beta-cystathionase as compared to wild-type levels. With use of this strain, an efficient three-step purification scheme is described that gives 90% pure enzyme in 54% yield with a specific activity of 215 IU/mg. This enzyme is characterized as to molecular weight (280 000), number of subunits (six), pyridoxal phosphate binding (5.7 mol of pyridoxal phosphate bound/mol of protein, Km of 0.005 mM), amino acid composition, substrate specificity, and kinetic properties.

Cloning, purification, and characterization of beta-cystathionase from Escherichia coli.

A series of derivatives of the phenylpyrrole fungicide fenpiclonil was synthesized in which a carboxyl group was present at various sites of this non-phloem-mobile molecule. Using the Kleier model, all these acidic analogues were predicted to be moderately phloem-mobile, especially the N-substituted derivatives. One of these latter molecules, N-carboxymethyl-3-cyano-4-(2,3-dichlorophenyl)pyrrole, exhibited some fungicidal activity on the pathogenic fungus Eutypa lata, and was then tested as a phloem-mobile pesticide in the Ricinus system. The compound was indeed mobile in the sieve tubes and was not degraded to fenpiclonil in the phloem sap under our experimental conditions. Its concentration in the sap was closely correlated to the percentage of the undissociated form of the molecule in the external medium, and was similar under acidic conditions (external pH 4.6-5.0) to that of the herbicide glyphosate.

/pdf/synthesis-and-phloem-mobility-of-acidic-derivatives-of-the-2vrz36fbq9.pdf

Synthesis and phloem mobility of acidic derivatives of the fungicide fenpiclonil

The title compound, an analogue of [Leu5]-enkephalin with L-o-carboranylalanine replacing L-phenylalanine in position 4, was prepared by fragment condensation. The analogue has a 3-fold higher affinity for rat brain opiate receptors in the [3H]naloxone competition assay than natural [Leu5]-enkephalin. Like [Leu5]-enkephalin and Na-acetyl-[Leu5]-enkephalin, the N-terminal tripeptide fragment, H · Tyr-Gly-Gly · OH, had no melanotropic activity in the Rana pipiens frog skin assay.



A convenient, direct synthesis of methyl t-butoxycarbonyl-L-propargylglycinate is described, and the 13C-NMR. spectra of L-o-carboranylalanine recorded. The procedure was extended to the preparation of BOC · Car-Leu · OMe from BOC · Pra-Leu · OMe. A number of new propargylglycine derivatives are reported.

The Synthesis of [4‐Carboranylalanine, 5‐Leucine]‐Enkephalin (Including an Improved Preparation of t‐Butoxycarbonyl‐L‐o‐carboranylalnine, New Derivatives of L‐Propargylglycine, and a Note on Melanotropic and Opiate Receptor Binding Characteristics)

The Syntheses and Microbiological Properties of Acetylenic Amino Acids. Propargylglycine and 2-Amino-3-methyl-4-pentynoic Acid1

Propargylglycine: an acetylenic amino acid antagonist

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The Syntheses and Microbiological Properties of Acetylenic Amino Acids. Propargylglycine and 2-Amino-3-methyl-4-pentynoic Acid1

Propargylglycine: an acetylenic amino acid antagonist